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  • 02월 19일 10시 이후 : 초록수정 불가능, 일정확인 및 검색만 가능

제121회 대한화학회 학술발표회, 총회 및 기기전시회 안내 Design and Synthesis of Novel Si-Rhodamine-Based NIR Fluorescent Probes for Development of Activity-Based Probe for in vivo Imaging of Hypoxia

2018년 2월 13일 16시 20분 36초
MEDI.P-664 이곳을 클릭하시면 발표코드에 대한 설명을 보실 수 있습니다.
4월 19일 (목요일) 11:00~12:30
Medicinal Chemistry
저자 및
KUNAL MORE, Dong-Jo Chang*
Department of Pharmacy, Suncheon National University, Korea
Hypoxia is one of the major characteristic of metastatic and solid tumors caused by an imbalance between oxygen consumption and supply leading to lack of oxygen. Status of hypoxia in solid tumors markedly influences their therapeutic responses to conventional anticancer therapies such as radiotherapy and chemotherapy due to altered tumor metabolism and angiogenesis. Thus, in vivo imaging of hypoxia is emerging as an important step to improve efficiency of anticancer therapy during anticancer drug development. Bioimaging of hypoxic biomarkers such as HIF-1, VEGF, carbonic anhydrase IX (CA-IX), glucose transporter 1 (GLUT-1) and reductive enzymes (nitroreductase, azoreductase and DT-diaphrose) are widely used for imaging of hypoxia. Many fluorescent probes have been discovered as an activity-based fluorescent probe for hypoxia imaging based on the ‘switch on’ fluorescence caused by the reduction of nitro group by nitroreductase (NTR) highly expressed in hypoxic cells. Although many studies are performed for an effective fluorescent probe for in vitro detection of NTR but still there is lack of techniques for in vivo imaging of hypoxia by NTR sensing. Near infrared (NIR) fluorophores are very desirable for in vivo imaging due to its excellent photo stability, high tissue transparency and low autofluorescence. NIR dyes such as cyanine dyes, Si-rhodamines and phosphinate-based red dyes are previously reported as promising fluorophores for imaging purpose but no probe was reported based on an NIR fluorophore for in vivo imaging of hypoxia. In this study, we have designed and synthesized novel NIR fluorophore based on Si-Rhodamine. These novel Si-rhodamine fluorophores are further developed by attaching NTR sensing moiety for detection of NTR under hypoxic condition.